NEW DISUBSTITUTED PHENYL PIPERIDINES/PIPERAZINES AS MODULATORS OF DOPAMINE NEUROTRANSMISSION Russian patent published in 2009 - IPC C07D211/18 C07D211/22 C07D211/52 C07D295/14 C07D295/06 A61K31/495 A61P25/00 

FIELD: chemistry.

SUBSTANCE: present invention refers to the new compounds of formula 1: whereat : X is N or CH; R₁ is selected from the group consisting of OSO₂CH₃, SOR₄, SO₂R₄, SO₂NH₂, SO₂NHCH₃, SO₂N(CH₃)₂, COR₄, CN, OCF₃, CF₃, F, Cl, Br, I, CH(OH)CF₃, CH₂SO₂CF₃, CH₂SO₂CH₃, CH₂CF₃, CH₂COCH₃, CH₂COCF₃; R₂ is selected from the group consisting of CN, CF₃, OH, OR4, F, CI, Br, I, CH₃; R₃ is selected from the group consisting of C₁-C₄ alkyls, allyl, CH₂CH₂OCH₃, CH₂CH₂CH₂F, CH₂CH₂CHF₂, CH₂CH₂F, CH₂CHF₂, CH₂CF₃, 3,3,3-trifluoropropyl, 4,4,4-trifluorobuthyl; CH₂CH₂OH, CH₂CH₂CH₂OH, CH₂CH(OH)CH₃, CH₂CH₂COCH₃, , ;

R₄ is selected from the group consisting of C₁-C₃ alkyls, CF₃, CHF₂, CH₂F; provided that when R₁ is CN, OCF₃, CF₃, F or Cl X is not CH, R₂ is not F, CI, Br, CH₃, and R₃ is not C₁-C₃ alkyl or allyl; provided that when R₁ is CF₃ or CN, X is not CH, R₂ is not F, CI, Br, CH₃, and R₃ is not C₁-C₂ alkyl; provided that when X is N: R₁ is not Cl, when R₂ is CH₃, and R₃ is CH₂CH₂OH; R₁ is not Cl, when R₂ is Cl, and R₃ is CH₃; R₁ is not F, when R₂ is CN, and R₃ is CH₃; R₁ is not Cl, when R₂ is Cl, and R₃ is CH₂CH₂CH₂OH; R₁ is not Cl, when R₂ is Cl, and R₃ is CH₂CH₂OH; and provided that when R₁ is SO₂R₄, SO₂NH₂, SO₂NHCH₃ or SO₂N(CH₃)₂ R₂ is not OH. The present invention refers also to the pharmaceutically acceptable salts of the said compounds, to the intermediate compounds, to their pharmaceutical composition as well as to the method of central nervous system abnormalities treatment.

EFFECT: obtaining of the new bioactive compounds active as modulators of dopamine neurotransmission.

43 cl, 79 ex, 7 tbl